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TMC310911 Sale

(Synonyms: ASC-09) 目录号 : GC65584

TMC310911 是一种有效且具有口服活性的 HIV-1 蛋白酶抑制剂,对于野生型 HIV-1,EC50 值范围为 2.2 nM 至 14.2 nM。TMC310911 对多种重组的 HIV-1 分离株也具有有效的活性,并具有很强的抗病毒活性。

TMC310911 Chemical Structure

Cas No.:1000287-05-7

规格 价格 库存 购买数量
1mg
¥765.00
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5mg
¥2,250.00
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10mg
¥3,960.00
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25mg
¥8,370.00
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Sample solution is provided at 25 µL, 10mM.

Description

TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity[1][2].

For a panel of 2,011 recombinant isolates with decreased susceptibility to at least one of the currently approved protease inhibitors (PIs), the FC in TMC310911 EC50 is ≤4 for 82% of isolates and ≤10 for 96% of isolates. The fold change (FC) in TMC310911 EC50 is ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to Darunavir, respectively. In vitro resistance selection (IVRS) performed with r13025, a multiple-PI-resistant recombinant isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC50 = 16)[1].The TMC310911 EC50 values against HIV-1/LAI and HIV-2/ROD in MT4 cells with EC50 values of 14.2 nM and 2 nM, respectively, and HIV-1/LAI and HIV-1/SF2 in PBMCs with EC50 values of 2.2 nM and 2.3 nM, respectively, and HIV-1/BaL in M/M cells with an EC50 value of 13.9 nM. And the corresponding EC90 values ranged from 5.0 to 94.7 nM. The TMC310911 CC50 for MT4 cells is 9.9 μM[1].

[1]. Dierynck I, et al. TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors. Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31.
[2]. Stellbrink HJ, et al. Antiviral activity, pharmacokinetics, and safety of the HIV-1 protease inhibitor TMC310911, coadministered with ritonavir, in treatment-naive HIV-1-infected patients. J Acquir Immune Defic Syndr. 2014 Mar 1;65(3):283-9.

化学性质

Cas No. 1000287-05-7 SDF Download SDF
别名 ASC-09
分子式 C38H53N5O7S2 分子量 755.99
溶解度 DMSO : 100 mg/mL (132.28 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.3228 mL 6.6138 mL 13.2277 mL
5 mM 0.2646 mL 1.3228 mL 2.6455 mL
10 mM 0.1323 mL 0.6614 mL 1.3228 mL
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